Vitamins and minerals may be broadly defined as substances that are essential for the maintenance of normal metabolic function but are not synthesized in the body. These substances must be furnished from an exogenous source. A healthy individual ingesting a well-balanced diet receives adequate amounts of vitamins and minerals from food. Vitamins obtained in this manner are not generally regarded as drugs.
However, there are many situations in which the concentration of one or more vitamins or minerals in the body tissues may be suboptimal. When such circumstances arise or can be anticipated, it is the common practice to administer vitamins or minerals in a chemically pure form. When employed in this manner, vitamins and minerals may be regarded as drugs and a knowledge of their pharmacological properties is desirable. For example, large doses of various vitamins are frequently employed for the treatment of disorders that are not etiologically related to vitamin deficiency. The implication is that such large doses may exert pharmacodynamic actions that are useful in therapy. It should be noted, however, that excessive administration of certain vitamins, notably vitamin A, can cause untoward toxic effects.
In today""s fast paced society many physicians and dieticians believe that a daily dietary vitamin and mineral supplement acts prophylactically to prevent pathologies associated with vitamin and mineral deficiencies. These supplements typically include several vitamins and minerals, and are referred to as multi-vitamin formulations. Examples of these preparations include One-A-Day(copyright) and Centrum(copyright) multi-vitamins. Researchers have suggested that multi-vitamins which include large quantities of vitamins and minerals are effective both for prophylactic purposes and for the treatment of an enormous variety of illnesses. Many millions of individuals living in the United States regularly ingest multi-vitamin preparations.
Some of these multi-vitamin preparations contain amounts of vitamins and minerals that are in excess of the RDA daily requirements. In the case of the water-soluble vitamins, there is little harm done to the body because of the low toxicity of this class of compounds. The low toxicity of the water-soluble vitamins is attributable to the fact that excess quantities of these substances are rapidly excreted in the urine. In the case of the lipid-soluble vitamins, the compounds accumulate in the body fat and can cause untoward toxic effects.
It is extremely important to distinguish between supplemental and therapeutic vitamin preparations. The latter contains much larger quantities of the individual vitamins and minerals than do the supplemental preparations. The present invention is directed to supplemental preparations.
The use of dietary multi-vitamin supplements should be considered by the physician in a wide variety of situations. Such situations may result from (1) inadequate vitamin intake, (2) mal-absorption syndromes, and (3) increased tissue requirements.
Vitamin deficiency due to an inadequate intake arises in a variety of circumstances. There are still large parts of the world and even considerable areas in the United States where, owing to poverty, the population eats a diet inadequate in terms of vitamin content. Moreover, there are areas where the prevalence in the diet of one particular type of food results in a relatively high incidence of vitamin deficiencies. Eccentric diets resulting from psychiatric disturbance, individual idiosyncrasies, religious beliefs, or food fads are other major causes of vitamin deficiency. A decrease in food consumption because of excess use of alcoholic beverages, poor appetite, dieting to combat obesity, or restricted diets prescribed by physicians for the management of specific diseases represents a further group of situations in which vitamin deficiency can arise.
A disturbance in absorption of vitamins is also seen in a variety of conditions. Examples are diseases of the liver and biliary tract, prolonged diarrhea from any cause, hyperthyroidism, pernicious anemia, and a variety of other disorders of the digestive system. Moreover, since a substantial proportion of certain vitamins is provided by the bacteria of the gastrointestinal tract, treatment with antimicrobials that alter the intestinal bacterial flora may lead inevitably to a decreased vitamin absorption.
Increased tissue requirements for vitamins also occur under a variety of conditions so that a nutritional deficiency may develop on a diet that had previously been adequate. Such situations can occur in both health and disease. In healthy individuals, for example, there is a greater requirement for various nutrients, including vitamins, during growth, during periods of hard physical work, exercise, during pregnancy, lactation, and menstruation. Diseases associated with an increased metabolism, such as hyperthyroidism, and conditions accompanied by fever or tissue wasting also increase the body""s requirements for vitamins. There is also good evidence that vitamin requirements increase during stress and after injury.
Multiple-vitamin therapy, using supplemental dietary multi-vitamins, is desirable in a variety of situations. Since deficiency of a single vitamin is rarely encountered clinically, it is customary practice in cases of suspected vitamin deficiency, as well as in prophylactic treatment, to recommend that multiple-vitamin therapy be administered. Typical of the multi-vitamins available are One-A-Day and Centrum multi-vitamins. (Table 3). Multi-vitamins such as these provide a great number of the essential vitamins and minerals needed by healthy individuals. Further, these preparations include electrolytes, and trace elements.
Recently, it has been determined that antioxidants, and free radical scavenging agents are protective against the development of certain cancers. Although, multi-vitamin preparations currently available include many needed vitamins and minerals, they do not include the antioxidants and/or free radical scavengers which have been shown to enhance the immune system and to prevent certain cancers, cardiovascular disorders, inflammatory diseases and to slow aging. Further, currently available multi-vitamin preparations do not include cardio-protective inositol or polyunsaturated fatty acids having an eicosapentaenoic acid: docosahexenoic acid ratio of about 18:12 commonly referred to as Omega-3 fish oils. Still further, several enzymes, amino acids, and dietary supplements which are known to be necessary and beneficial in supplementing an individual""s diet are not included in presently available multi-vitamin formulations. Accordingly, a new multi-vitamin dietary supplement is needed which incorporates many of these beneficial ingredients into a stable pharmaceutical preparation.
The U.S. Pat. No. 4,599,234 issued to Amer, Jul. 8, 1986, describes a diet comprising a source of selenium, butylated hydroxytoluene or butylated hydroxyanisole, and xcex2-carotene that reduces the effect of carcinogens presented in the diet. The issued claims indicate a weight ratio of selenium:BHT:xcex2-carotene of 1:0.5:0.05. In contrast, the optimal ratio of these ingredients in the formulation of the present invention is 1:2000:120. Taking into account the range of concentrations of these ingredients indicated in this invention, the closest ratio to that of Amer is 1:100:15.
The U.S. patent issued to Newmark (4,022,913) May 10, 1977 describes high potency compositions of vitamin A acetate and/or vitamin A alcohol stabilized against the formation of crystals by vitamin A palmitate. The compositions can contain antioxidants such as BHA, BHT propyl gallate, Vitamin E, and Vitamin C which are customarily utilized as a preservative in this type of preparation. Newmark does not teach that any of these antioxidants are cancer-protective.
The present invention concerns development of a multi-vitamin dietary supplement formulation which includes several dietary supplements which are cancer-protective. By including cancer- and cardio-protective immunostimulatory compounds in a multi-vitamin formulation, the present invention advantageously provides the general population the benefits of recent scientific research which has discovered that several agents are, for example, cancer- and cardio-protective. Accordingly, it is believed that the inventive methods and formulations will provide the general population with an improved multi-vitamin formulation capable of reducing the incidence of diseases such as cancer and heart disease while enhancing longevity and the immune system.
In still another aspect of the present invention, a method of inhibiting tumor-promoting effects of carcinogens in an animal is provided, the method comprising the administration of a daily dietary supplement at prophylactically effective levels including the formulation of the present invention.
Previous to the formulation of the present invention, no one had demonstrated the efficacy of these particular ingredients or the ratio of these particular ingredients of the present formulation in inhibiting the tumor-promoting effects of carcinogens in animals.
The present invention is directed to a formulation including vitamins, minerals and other beneficial supplements that is demonstrated to be cancer-protective. More specifically, the invention is directed to a formulation and methods of manufacturing and administering prophylactically effective amounts of a formulation containing vitamins and minerals in association with antioxidants, polyunsaturated fatty acids having an eicosapentaenoic acid:docosahexenoic acid ratio of about 18:12, food concentrate containing naturally occurring anti-oxidizing enzymes such as catalase and superoxide dismutase, for example, and amino acids. The formulations of the present invention exploit novel synergistic relationships which have not previously been reported in the inhibition of the induction of tumors, inhibition of spontaneous tumor formation and increase in lifespan.
One aspect of the present invention is directed to a daily multi-vitamin and mineral dietary supplement which comprises BHA or BHT, propyl gallate, Vitamin E, Vitamin C, xcex2-carotene, and Selenium. Combinations of these ingredients are shown to inhibit tumor-promoting effects of carcinogens in an animal.
Several of the antioxidants, vitamins and minerals contained in the formulation have been shown to inhibit the induction of cancer at several stages in the multistage process. For example, B-carotene, glutathione, cysteine, BHA, BHT, Vitamins A, C and E, as well as selenium, inhibit the tumor initiation, promotion and progression stages of cancer. The heretofore unrecognized synergistic effects of BHA and Vitamin E, for example, may be related to the observations that BHA inhibits tumor promoter-induced polyamine synthesis, and that Vitamin E inhibits promoter-induced hyperplasia, thus leading to a synergistic effect. Furthermore, Vitamins A, C and E, selenium, BHA, BHT, and propyl gallate inhibit tumor initiation by counteracting the covalent binding of carcinogen to DNA and the mutagenic effect of carcinogens.
A further aspect of the present invention is directed to a multi-vitamin and mineral supplement including antioxidants in combination with certain preferred amino acids selected from the group consisting of reduced L-glutathione, L-cysteine, methionine, glutamine, and taurine. According to a preferred embodiment, the present inventive formulation further includes at least one of the following beneficial ingredients: polyunsaturated fatty acids having an eicosapentaenoic acid:docosahexenoic acid ratio of about 18:12, para-aminobenzoic acid, superoxide dismutase, catalase (these two enzymes being preferably obtained from a food concentrate), a citrus bioflavonoid, and inositol. Preferably, the reduced L-glutathione and the polyunsaturated fatty acids are microencapsulated in the present inventive formulation.
Preferably, the supplement of the present invention includes (but is not limited to) the following vitamins and minerals in an amount equal to or greater than the minimum daily requirement in man: folic acid, vitamin B1, vitamin B2, niacinamide, vitamin B6, vitamin B12, vitamin D3, biotin, pantothenic acid, vitamin K1, calcium, iodine, potassium, iron, magnesium, copper, zinc, manganese, chromium, molybdenum, vanadium, silicon, and boron.
An important aspect of the present invention is directed to a method of inhibiting tumor-promoting effects of carcinogens as well as increasing longevity and augmenting the immune system in an animal. The method includes the step of administering prophylactically effective amounts of (preferably daily) a dietary multi-vitamin and mineral supplement including antioxidants and other beneficial substances of the present invention at prophylactically effective levels. A prophylactically effective amount is an amount sufficient to inhibit said tumor promotion by carcinogens in an animal.
A still further aspect of the present invention is directed to the production of a sustained-release tableted dietary supplement which is intended to be administered one to three times daily.